期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 12, 页码 3828-3831出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.03.012
关键词
Vasopressin 1b; V1b; SSR149415; Oxindole; Metabolic stability
Herein we report the discovery of a novel series of vasopressin 1b (V1b) receptor antagonists, starting from potent but metabolically labile oxindole SSR149415. Masking the proline N,N-dimethyl amide moiety as an oxazole and attaching a benzylic amine moiety to the northern phenyl ring resulted in potent and selective V1b receptor antagonists with improved metabolic stability and improved pharmacokinetic properties in rat. Compound 18c was found to be efficacious in a rat model of anti-depressant activity. (C) 2011 Elsevier Ltd. All rights reserved.
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